PMID- 23293517 OWN - NLM STAT- MEDLINE DCOM- 20130916 LR - 20211021 IS - 1178-2013 (Electronic) IS - 1176-9114 (Print) IS - 1176-9114 (Linking) VI - 8 DP - 2013 TI - Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats. PG - 23-32 LID - 10.2147/IJN.S38507 [doi] AB - This study aimed to prepare nanoemulsions coated with alginate/chitosan for oral insulin delivery. Uncoated nanoemulsions were prepared by homogenization of a water in oil in water (w/o/w) multiple emulsion that was composed of Labrafac((R)) CC, phospholipid, Span 80 and Cremorphor((R)) EL. Coating of the nanoemulsions was achieved based on polyelectrolyte cross-linking, with sequential addition of calcium chloride and chitosan to the bulk nanoemulsion dispersion that contained alginate. The particle size of the coated nanoemulsions was about 488 nm and the insulin entrapment ratio was 47.3%. Circular dichroism spectroscopy proved conformational stability of insulin against the preparative stress. In vitro leakage study indicated well-preserved integrity of the nanoemulsions in simulated gastric juices. Hypoglycemic effects were observed in both normal and diabetic rats. The relative pharmacological bioavailability of the coated nanoemulsion with 25 and 50 IU/kg insulin were 8.42% and 5.72% in normal rats and 8.19% and 7.84% in diabetic rats, respectively. Moreover, there were significantly prolonged hypoglycemic effects after oral administration of the coated nanoemulsions compared with subcutaneous (sc) insulin. In conclusion, the nanoemulsion coated with alginate/chitosan was a potential delivery system for oral delivery of polypeptides and proteins. FAU - Li, Xiaoyang AU - Li X AD - Key Laboratory of Smart Drug Delivery of Ministry of Education and People's Liberation Army (PLA), School of Pharmacy, Fudan University, Shanghai, China. FAU - Qi, Jianping AU - Qi J FAU - Xie, Yunchang AU - Xie Y FAU - Zhang, Xi AU - Zhang X FAU - Hu, Shunwen AU - Hu S FAU - Xu, Ying AU - Xu Y FAU - Lu, Yi AU - Lu Y FAU - Wu, Wei AU - Wu W LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20121228 PL - New Zealand TA - Int J Nanomedicine JT - International journal of nanomedicine JID - 101263847 RN - 0 (Alginates) RN - 0 (Blood Glucose) RN - 0 (Drug Carriers) RN - 0 (Emulsions) RN - 0 (Hexuronic Acids) RN - 0 (Hypoglycemic Agents) RN - 0 (Insulin) RN - 8A5D83Q4RW (Glucuronic Acid) RN - 9012-76-4 (Chitosan) SB - IM MH - Administration, Oral MH - Alginates/administration & dosage/chemistry/pharmacokinetics MH - Analysis of Variance MH - Animals MH - Blood Glucose/drug effects/metabolism MH - Chitosan/administration & dosage/chemistry/pharmacokinetics MH - Circular Dichroism MH - Diabetes Mellitus, Experimental/blood/drug therapy/metabolism MH - Drug Carriers/administration & dosage/*chemistry/pharmacokinetics MH - Drug Stability MH - Emulsions/administration & dosage/*chemistry/pharmacokinetics MH - Gastric Juice/metabolism MH - Glucuronic Acid/administration & dosage/chemistry/pharmacokinetics MH - Hexuronic Acids/administration & dosage/chemistry/pharmacokinetics MH - Hypoglycemic Agents/*administration & dosage/*chemistry/pharmacokinetics MH - Insulin/*administration & dosage/chemistry/pharmacokinetics MH - Male MH - Models, Biological MH - Nanoparticles/administration & dosage/*chemistry MH - Particle Size MH - Rats MH - Rats, Wistar PMC - PMC3534302 OTO - NOTNLM OT - alginate OT - chitosan OT - insulin OT - nanoemulsion OT - oral delivery EDAT- 2013/01/08 06:00 MHDA- 2013/09/17 06:00 PMCR- 2012/12/28 CRDT- 2013/01/08 06:00 PHST- 2013/01/08 06:00 [entrez] PHST- 2013/01/08 06:00 [pubmed] PHST- 2013/09/17 06:00 [medline] PHST- 2012/12/28 00:00 [pmc-release] AID - ijn-8-023 [pii] AID - 10.2147/IJN.S38507 [doi] PST - ppublish SO - Int J Nanomedicine. 2013;8:23-32. doi: 10.2147/IJN.S38507. Epub 2012 Dec 28.